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Category:
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7TM Receptors Peptides (Neuropeptides)Tachykinin ReceptorsNK-1 Receptor
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Cat.No.
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Product Name
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2400 |
FK 888
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Price and Availability
Click here for full price details of
FK 888
Other Information:
Sold with the permission of Astellas Pharma Inc.
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Chemical Name:
(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-p
rolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-al
aninamide |
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Biological Activity:
Selective, high affinity tachykinin NK1
receptor antagonist (Ki = 0.69 nM) that displays 320-fold
selectivity for human over rat NK1 receptors. Inhibits substance
P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM)
and inhibits substance P-induced airway constriction in vivo following i.v. and
oral administration.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Fujii et al
(1992) Pharmacological profile of a high affinity dipeptide NK1
receptor antagonist. Br.J.Pharmacol. 107 785. Murai et
al (1993) Effects of an NK1 receptor antagonist, FK888, on
constriction and plasma extravasation induced in guinea pig airway by
neurokinins and capsaicin. Eur.J.Pharmacol. 236 7. Aramori et
al (1994) Subtype- and species-selectivity of a tachykinin receptor
antagonist, FK888, for cloned rat and human tachykinin receptors.
Eur.J.Pharmacol. 269 277.
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Keywords: FK 888, Peptides (Neuropeptides), High Affinity NK1 Receptor Antagonist, FK888, Tocris Bioscience
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